Details of the Drug Metabolized by Drug-Metabolizing Enzyme (DME)

General Information of Drug (ID: DR0569)
Drug Name
Eltrombopag olamine
Synonyms
EltroMbopag diethanolaMine salt; Eltrombopag (Olamine); Eltrombopag olamine; Eltrombopag olamine (JAN/USAN); Eltrombopag olamine [USAN:JAN]; Eltrombopag-SB-497115-GR; FT-0773802; HY-15306A; MFCD22380664; PLILLUUXAVKBPY-SBIAVEDLSA-N; Promacta; Promacta (TN); Promacta Olamine; Revolade; SB 497115GR; SB-497115-GR; SB-497115GR; SB19102; SCHEMBL16207741; SCHEMBL210183; UNII-4U07F515LG; Z-3296; 3608AH; 496775-62-3; 4U07F515LG; AC-26286; AKOS025396658; BCP07055; C25H22N4O4.2C2H7NO; CHEMBL3989691; CHEMBL4097947; CS-1566; D03978
Indication Thrombocytopenia [ICD11: 3B64] Approved [1]
Structure
3D MOL is unavailable 2D MOL
Pharmaceutical Properties Molecular Weight 564.6 Topological Polar Surface Area 207
Heavy Atom Count 41 Rotatable Bond Count 7
Hydrogen Bond Donor Count 7 Hydrogen Bond Acceptor Count 11
Cross-matching ID
PubChem CID
135449331
CAS Number
496775-62-3
TTD Drug ID
D00PEH
Formula
C29H36N6O6
Canonical SMILES
CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)N=NC3=CC=CC(=C3O)C4=CC(=CC=C4)C(=O)O)C.C(CO)N.C(CO)N
InChI
1S/C25H22N4O4.2C2H7NO/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33;2*3-1-2-4/h4-13,28,30H,1-3H3,(H,32,33);2*4H,1-3H2
InChIKey
DJMJHIKGMVJYCW-UHFFFAOYSA-N
The Metabolic Roadmap of This Drug
The Full List of Drug Metabolites (DM) of This Drug
DM Name DM ID PubChem ID Reaction DM Level REF
Eltrombopag olamine glucuronide conjugate DM000575 N. A. Conjugation - Glucuronidation 1 [2]
Mono-oxygenation DM000574 N. A. Oxidation - Oxidation 1 [2]
The Full List of Metabolic Reaction (MR) of This Drug
MR ID Reactant Product MR Type DME REF
MR000906 Eltrombopag olamine Mono-oxygenation Oxidation - Oxidation CYP1A2 ... [2]
MR000907 Eltrombopag olamine Eltrombopag olamine glucuronide conjugate Conjugation - Glucuronidation UGT1A1 ... [2]
Drug-Metabolizing Enzyme(s) (DME) Metabolizing This Drug
DME Name DME Info Species Uniprot ID EC Number REF
Cytochrome P450 1A2 (CYP1A2) DME0003 Homo sapiens
CP1A2_HUMAN
1.14.14.1
[2]
Cytochrome P450 2C8 (CYP2C8) DME0018 Homo sapiens
CP2C8_HUMAN
1.14.14.1
[3]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME0004 Homo sapiens
UD11_HUMAN
2.4.1.17
[3]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DME0041 Homo sapiens
UD13_HUMAN
2.4.1.17
[4]
References
1 Eltrombopag Olamine was approved by FDA. The 2020 official website of the U.S. Food and Drug Administration.
2 Eltrombopag for use in children with immune thrombocytopenia. Blood Adv. 2018 Feb 27;2(4):454-461.
3 Eltrombopag-induced acute liver failure in a pediatric patient: a pharmacokinetic and pharmacogenetic analysis. Ther Drug Monit. 2018 Aug;40(4):386-388.
4 Eltrombopag for use in children with immune thrombocytopenia Blood Adv. 2018 Feb 27;2(4):454-461. doi: 10.1182/bloodadvances.2017010660.

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